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Ketoprofen gel and preparation method thereof

A technology of gel and gel matrix, which is applied in the field of ketoprofen gel and its preparation, can solve the problems of expensive imported drugs and unacceptable by the general public, and achieve excellent analgesic and anti-inflammatory effects and good transdermal effect , quick effect

Inactive Publication Date: 2013-06-19
HANGZHOU SHARPLY PHARM R&D INSTIT +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For this defect of ketoprofen, ketoprofen is generally made into percutaneous absorption gel abroad. On the one hand, it can reduce the amount of ketoprofen medicine entering the body circulation and avoid it from stimulating the gastrointestinal tract. , improve the concentration of ketoprofen medicine at the site of action to achieve the purpose of analgesia, anti-inflammation and prolonging the drug effect, such as: Fastum of Italy Menarini Company, Oruvail of Spain Sanofi-aventis Company and Ricfen of Korea Hanmi Company, etc., but Imported drugs are expensive and unacceptable to the general public

Method used

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  • Ketoprofen gel and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Preparation formula: Ketoprofen 2.5g; Carbomer 941 0.8g; Menthol 0.04g; 95% ethanol 24.3g; Triethanolamine 0.14g; Sodium sulfite 0.2g; Purified water 72.0g.

[0016] Preparation process: Add 47.0g of purified water and 15.5g of 95% ethanol into a beaker, slowly add 0.8g of Carbomer 941 in batches, stir, and let it stand overnight to fully swell to obtain the gel matrix (a); Dissolve 2.5g of ketoprofen in 8.8g of 95% ethanol and 17.5g of purified water, and stir evenly to obtain solution (b); slowly add (b) into (a) while stirring, then add 0.04g of menthol and 0.2g sodium sulfite, stir to make it uniform; take the above solution, add an appropriate amount of triethanolamine while stirring, adjust the pH to about 7.0, and obtain the gel.

Embodiment 2

[0018] Preparation formula: ketoprofen 2.5g; carbomer 934 1.0g; citric acid 0.04g; 95% ethanol 24.3g; triethanolamine 0.2g; sodium sulfite 0.2g; purified water 72.0g.

[0019] Preparation process: Add 47.0g of purified water and 15.5g of 95% ethanol into a beaker, slowly add 1.0g of Carbomer 934 in batches, stir, and let it stand overnight to fully swell to obtain the gel matrix (a); Dissolve 2.5g of ketoprofen in 8.8g of 95% ethanol and 17.5g of purified water, and stir evenly to obtain solution (b); slowly add (b) into (a) while stirring, then add 0.04g of citric acid and 0.2g sodium sulfite, stir to make it uniform; take the above solution, add an appropriate amount of triethanolamine while stirring, adjust the pH to about 7.0, and obtain the gel.

Embodiment 3

[0021] Preparation formula: 2.5g of ketoprofen; 1.2g of poloxamer F68; 0.04g of menthol; 24.3g of 95% ethanol; 0.2g of sodium sulfite; 71.8g of purified water.

[0022] Preparation process: Add 47.0g of purified water and 15.5g of 95% ethanol into a beaker, slowly add 1.2g of poloxamer F68 in batches, and stir evenly to obtain a gel matrix (a); then dissolve 2.5g of ketoprofen In 8.8g of 95% ethanol and 17.3g of purified water, stir evenly to obtain solution (b); slowly add (b) into (a) under stirring, then add 0.04g of menthol and 0.2g of sodium sulfite, stir to make Uniform, that is, the gel.

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Abstract

The invention relates to a ketoprofen gel and a preparation method thereof. The ketoprofen gel is prepared from the following components: 2-5 % of ketoprofen, 0.5-2 % of matrix material, 2-4 % of a transdermal enhancer, 0.5-5 % of a neutralizer, 0.05-0.2 % of an anti-oxidant, 20-50 % of ethanol and the balance being water. The ketoprofen gel provided by the invention solves problems of stimulation of ketoprofen preparations on gastrointestinal tract in a background technology, is used externally, has advantages of good transdermal effect, quick effect and good analgesic and anti-inflammatory effects, and can play drug effects for a long time.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to ketoprofen gel and a preparation method thereof. Background technique [0002] Ketoprofen (KP) is a phenylpropionic acid non-steroidal anti-inflammatory analgesic drug. For gout and other diseases, ketoprofen is also effective for trauma and postoperative pain. The dosage is small, the toxicity is low, the curative effect is high, and the effect is rapid and lasting. Studies have found that under the same dosage conditions, the analgesic and anti-inflammatory effects of ketoprofen are 150 times stronger than that of aspirin, and the analgesic effect is 3.75 times that of diclofenac sodium. Oral administration of ketoprofen has a first-pass effect, and may cause gastrointestinal side effects at the same time, which is not conducive to long-term medication. In addition, in the conventional dose, if the relative risk of ibuprofen to the gastrointestinal tract is set as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/192A61P29/00
Inventor 范敏华高剑利刘华
Owner HANGZHOU SHARPLY PHARM R&D INSTIT
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